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Antihistamines Pharmacology

Antihistamines block the effects of histamine in the body and are used to treat allergy symptoms and other conditions. They work by antagonizing H1 and H2 receptors. First generation antihistamines have sedative effects while second generation mainly have antihistaminic effects. Common brands include Benadryl, Claritin, Zyrtec and Pepcid with recommended dosages provided.
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0% found this document useful (0 votes)
80 views10 pages

Antihistamines Pharmacology

Antihistamines block the effects of histamine in the body and are used to treat allergy symptoms and other conditions. They work by antagonizing H1 and H2 receptors. First generation antihistamines have sedative effects while second generation mainly have antihistaminic effects. Common brands include Benadryl, Claritin, Zyrtec and Pepcid with recommended dosages provided.
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ANTIHISTAMINES

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WHAT IS ANTIHISTAMINES?

An antihistamine is a prescription or over-the-


counter medication that blocks some of what
histamine does.
HOW DOES ANTIHISTAMINES
WORK?

An Antihistamines block the effects of a substance


called histamine in your body. Histamine is
normally released when your body detects
something harmful, such as an infection. It causes
blood vessels to expand and the skin to swell,
which helps protect the body.
MECHANISM OF ACTION
Histamine (an endogenous chemical messenger) induces
an increased level of vascular permeability, which leads
to fluid moving from capillaries into the surrounding
tissues. The overall outcome of this is increased swelling
and dilation of vessels. Antihistamines stop this effect by
acting as antagonists at the H-1 receptors. The clinical
benefit is a reduction in allergy symptoms and any
related symptoms.
CLASSIFICATION OF ANTIHISTAMINES

 H-1 receptor antagonists or H-1 blockers. This subtype of


antihistamines is used to treat allergy symptoms. The H-1
blocker subtype is further broken down into two groups — first-
generation antihistamines and second-generation
antihistamines.

 H-2 receptor antagonists or H-2 blockers. They are used to treat


gastrointestinal conditions, including gastroesophageal reflux
disease [GERD] (also called acid reflux), peptic ulcers, gastritis,
motion sickness, nausea and vomiting.
DIFFERENCE BETWEEN FIRST AND SECOND
GENERATION ANTIHISTAMINES

 FIRST-GENERATION ANTIHISTAMINES- beside their antihistaminic


effect (neutralizing allergy, itching, edema), they have sedative
effect for (for pain and sleep), antiemetic effect (for nausea and
vomiting), and anticholinergic effect (for runny nose).

 SECOND-GENERATION ANTIHISTAMINES- have mainly


antihistaminic effect, ,with no or very little sedation,
anticholinergic, antiemetic effects
ANTIHISTAMINES BRAND EXAMPLES AND
RECOMMENDED DOSAGE
Examples of first-generation over-the-counter and prescription H-1 blockers
BRAND NAMES RECOMMENDED DOSAGE

Brompheniramine (Children’s 10mL every 4 hours; max 6 doses/24 hours


Dimetapp Cold®)
Chlorpheniramine (Chlor-Trimeton®) One tablet every 4-6 hours, not to exceed 6 tablets in
24 hours
Clemastine (Dayhist®) 1.34 mg PO q12hr; not to exceed 8.04 mg/day for
syrup or 2.68 mg/24 hours for tablets
Cyproheptadine (Periactin®) 4 mg PO q8hr initially

Dexchlorpheniramine Dimenhydrinate 50-100 mg PO/IV/IM q4-6hr PRN


(Dramamine®)
Diphenhydramine (Benadryl®) 25-50 mg every 4-6 hours.
ANTIHISTAMINES BRAND EXAMPLES AND
RECOMMENDED DOSAGE
Examples of second-generation over-the-counter and prescription H-1 blockers

BRAND NAMES RECOMMENDED DOSAGE

Azelastine (Astelin®) 1-2 sprays per nostril q12hr

Loratadine (Claritin®) 10 mg PO qDay

Cetirizine (Zyrtec®) 10 mg PO qDay

Desloratadine (Clarinex®) 5 mg PO qDay

Fexofenadine (Allegra®) 180 mg PO qDay or 60 mg PO BID


ANTIHISTAMINES BRAND EXAMPLES AND
RECOMMENDED DOSAGE
Examples of H-2 antihistamines
BRAND NAMES RECOMMENDED DOSAGE

Cimetidine (Tagamet HB®) 800 mg PO qHS OR. 400 mg PO q12hr OR. 300 mg
PO q6hr.

Famotidine (Pepcid®) 20 mg PO/IV q12hr or 40 mg PO at bedtime

Nizatidine (Axid®) 300 mg PO qHS OR. 150 mg PO q12hr.

Ranitidine (Zantac®) 150mg twice daily or 300mg once daily after


evening meal or at bedtime
DENTAL CONSIDERATION

 Anti-histamines are medication that relieve inflammation and


sometimes used in dental practice to relieve inflammatory-
caused pain.

 Antihistamines also block the release of saliva, which results in


dry mouth and can increase the risk for cavities.

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